Abstract The field of drug metabolism is at the frontier of predicting human drug disposition (absorption, distribution, metabolism, and elimination or ADME) and safety/toxicity from cellular and pre-clinical data. Clinical safety and efficacy of drug is especially critical to predict accurately in vulnerable populations such as pediatric and understudied populations. To this end, it is critical to constantly fill knowledge gaps in the translation of new basic science knowledge into clinical use. The 2018 Drug Metabolism Gordon Research Conference (GRC) will fill a major gap in addressing these critical issues to achieve the goals of ADME and toxicity prediction that are of particular relevance to drug development scientists in the drug metabolism/transport and pharmacokinetics/pharmacodynamics (DMPK) field. The conference will focus on new basic science on drug metabolizing enzymes, transporters, and interaction between the cell membrane and these proteins. The second half of the conference will connect this basic science to clinical studies with drug-drug interactions, DMPK in special populations, and regulatory guidelines and case studies in the clinic. The goal of this conference is to provide a stimulating and collaborative environment for translational researchers to openly discuss unpublished work, push the boundaries of science, and foster scientific interactions between young investigators, leaders in the field, and colleagues working in academia, the pharmaceutical industry and regulatory agencies. This conference will bring together scientists with expertise in diverse disciplines that are fundamental to drug metabolism and clinical DMPK to discuss recent scientific advances and applications in predicting human drug ADME and toxicity. Conferees will learn about technological advances and transformative approaches in drug metabolizing enzyme and transporter structure, function, and role in drug disposition and toxicity, discuss challenges, and consider strategies to overcome hurdles. This conference will provide a forum for graduate students and postdoctoral fellows to expand their scientific breadth, interact with leaders in the field, establish future collaborative relationships, and consider various career paths. The lectures are held in the mornings and evenings with the afternoons available for informal discussions and recreation. GRC meetings are small and designed for more discussion time during both the formal scientific sessions and during informal interactions (e.g., poster sessions, meal times, afternoon outings). To facilitate ample opportunity to discuss their work, the Drug Metabolism GRC organizes four, 2-hour poster sessions, with each poster presenter (at least 60) available for discussion during two sessions.